发明授权
- 专利标题: Ketone derivatives
- 专利标题(中): 酮酮衍生物
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申请号: US651016申请日: 1991-02-04
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公开(公告)号: US5084474A公开(公告)日: 1992-01-28
- 发明人: Alexander W. Oxford , David J. Cavalla , Peter C. North
- 申请人: Alexander W. Oxford , David J. Cavalla , Peter C. North
- 申请人地址: GB2 London
- 专利权人: Glaxo Group Limited
- 当前专利权人: Glaxo Group Limited
- 当前专利权人地址: GB2 London
- 优先权: GBX8708943 19870414; GBX8713226 19870605; GBX8713227 19870605; GBX8716698 19870715; GBX8720694 19870903
- 主分类号: A61K31/47
- IPC分类号: A61K31/47 ; A61P1/00 ; A61P1/04 ; A61P1/08 ; A61P25/04 ; A61P25/18 ; C07D233/54 ; C07D233/64 ; C07D401/06 ; C07D403/06 ; C07D405/06 ; C07D409/06 ; C07D471/04
摘要:
The present invention provides ketones of the general formula (I): ##STR1## and physiologically acceptable salts and solvates thereof, wherein R.sup.1 and R.sup.2, which may be the same or different, each represents a hydrogen atom or a C.sub.1-6 alkyl group; Im represents an imidazolyl group of formula: ##STR2## wherein one of the groups represented by R.sup.3, R.sup.4 and R.sup.5 is a hydrogen atom or a C.sub.1-6 alkyl, C.sub.3-7 cycloalkyl, C.sub.3-6 alkenyl, phenyl or phenylC.sub.1-3 alkyl group, and each of the other two groups, which may be the same or different, represents a hydrogen atom or a C.sub.1-6 alkyl group; andA is a group of the formula (a), (b), (c), (d), (e), (f) or (g) as set forth hereinafter,and when A is the group (g), the group --COCR.sup.1 R.sup.2 CH.sub.2 Im is attached at the 2- or 4- position of the indole moiety.The compounds are potent and selective antagonists of the effect of 5-HT at 5-HT.sub.3 receptors and are useful, for example, in the treatment of psychotic disorders, anxiety and nausea and vomiting.
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